专利号:US-10759743-B2 优先权日:2016-10-24 标 题 :Pd-catalyzed γ-C(sp3)-H arylation / heteroarylation of free amines 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
专利号:US-5496952-A 优先权日:1995-02-07 标题 :Method of making asymmetric DE ring intermediates for the synthesis of camptothecin and camptothecin analogs 发明人:COMINS DANIEL L 权利人:UNIV NORTH CAROLINA STATE 摘要:The present invention is directed towards new methods of making DE ring intermediates of Formula (III), ##STR1## wherein Y is H or halogen and R is loweralkyl, which in turn are useful in methods of making camptothecin and camptothecin analogs. The present invention also provides new compounds useful in the methods of making compounds of Formula (III).
专利号:WO-2024044825-A1 优先权日:2022-09-01 标 题:Compound collections, compounds and synthesis thereof 发明人:FLYNN BERNARD; CHEN SHUQI; PRIEBBENOW DANIEL; JASZEWSKI LEO 权利人:UNIV MONASH 摘要:Provided herein are collections of compounds of formula a) to u), and salts thereof, which have polycyclic aromatic scaffolds and thus have structures targeted towards binding polynucleotide therapeutic targets, including polynucleotide-protein complexes. Also provided are compounds and salts themselves, methods of synthesizing such compounds, methods of identifying compounds having activity against a polynucleotide target, use of the compounds as reference compounds in assays, and phenotypic methods of identifying a new polynucleotide target using the compounds.
专利号:US-6552018-B1 优先权日:1997-01-27 标 题:Pyrazole derivatives 发明人:EJIMA AKIO; OHSUKI SATORU; OHKI HITOSHI; NAITO HIROYUKI 权利人:DAIICHI SEIYAKU CO 摘要:The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): n wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: n These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)- 1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.
专利号:US-8828907-B2 优先权日:2009-03-25 标题:Active ingredient combinations having insecticidal and acaricidal properties 发明人:HUNGENBERG HEIKE; JESCHKE PETER; VELTEN ROBERT; THIELERT WOLFGANG 权利人:HUNGENBERG HEIKE; JESCHKE PETER; VELTEN ROBERT; THIELERT WOLFGANG; BAYER CROPSCIENCE AG 摘要:The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) n nin whichn nR 1 and A have the meanings given in the descriptionn nand, secondly, at least one further known active compound from the class of the chitin synthesis inhibitors, the molting hormone agonists or other classes, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids.
专利号:CN-117024334-A 优先权日:2023-07-20 标 题:A kind of synthesis method of 2-fluoro-3-hydroxypyridine